KJ Pyr 9 (KJ-Pyr-9) acts by disrupting the MYC-MAX complex formation within cells, as observed in protein fragment complementation assays[1]. KJ Pyr 9 specifically targets and inhibits MYC-induced oncogenic transformation in cell cultures, showing minimal or negligible impact on the oncogenic functions of various unrelated oncoproteins[1]. KJ Pyr 9 notably affects the proliferation of cells overexpressing MYC, both human and avian, and distinctively reduces the transcriptional signature driven by MYC[1]. KJ Pyr 9 efficacy has been tested against three cell lines known for their dependence on enhanced MYC activity: NCI-H460, MDA-MB-231, and SUM-159PT, successfully inhibiting their proliferation with IC50 values ranging between 5 and 10 μM[1]. Burkitt lymphoma cell lines, characterized by constitutively high c-MYC expression, show even greater sensitivity to KJ Pyr 9, with IC50 values between 1 and 2.5 μM[1].
体内研究
Additionally, KJ Pyr 9 administered intraperitoneally at 10 mg/kg daily for 31 days has been found capable of arresting tumor growth[1].
体外研究
KJ Pyr 9 (KJ-Pyr-9) acts by disrupting the MYC-MAX complex formation within cells, as observed in protein fragment complementation assays[1].
KJ Pyr 9 specifically targets and inhibits MYC-induced oncogenic transformation in cell cultures, showing minimal or negligible impact on the oncogenic functions of various unrelated oncoproteins[1].
KJ Pyr 9 notably affects the proliferation of cells overexpressing MYC, both human and avian, and distinctively reduces the transcriptional signature driven by MYC[1].
KJ Pyr 9 efficacy has been tested against three cell lines known for their dependence on enhanced MYC activity: NCI-H460, MDA-MB-231, and SUM-159PT, successfully inhibiting their proliferation with IC50 values ranging between 5 and 10 μM[1].
Burkitt lymphoma cell lines, characterized by constitutively high c-MYC expression, show even greater sensitivity to KJ Pyr 9, with IC50 values between 1 and 2.5 μM[1].
KJ Pyr 9 细胞实验
Cell Line
Concentration
Treated Time
Description
References
LXF-289
1, 5, 10, 20 µM
5 days
Inhibition of the protein–protein interaction of MYC/NMYC with MAX, significantly reducing cell survival
Cells. 2021 Apr 27;10(5):1024
BKZ-9
1, 5, 10, 20 µM
5 days
Inhibition of the protein–protein interaction of MYC/NMYC with MAX, significantly reducing cell survival
Cells. 2021 Apr 27;10(5):1024
BKZ-8
1, 5, 10, 20 µM
5 days
Inhibition of the protein–protein interaction of MYC/NMYC with MAX, significantly reducing cell survival
Cells. 2021 Apr 27;10(5):1024
BKZ-7
1, 5, 10, 20 µM
5 days
Inhibition of the protein–protein interaction of MYC/NMYC with MAX, significantly reducing cell survival
Cells. 2021 Apr 27;10(5):1024
BKZ-6
1, 5, 10, 20 µM
5 days
Inhibition of the protein–protein interaction of MYC/NMYC with MAX, significantly reducing cell survival
Cells. 2021 Apr 27;10(5):1024
BKZ-5
1, 5, 10, 20 µM
5 days
Inhibition of the protein–protein interaction of MYC/NMYC with MAX, significantly reducing cell survival
Cells. 2021 Apr 27;10(5):1024
BKZ-4
1, 5, 10, 20 µM
5 days
Inhibition of the protein–protein interaction of MYC/NMYC with MAX, significantly reducing cell survival
Cells. 2021 Apr 27;10(5):1024
RCH-ACV cells
8 μM
60 hours
To evaluate the effect of KJ-Pyr-9 on the proliferation and apoptosis of RCH-ACV cells, results showed that KJ-Pyr-9 significantly inhibited cell proliferation and increased apoptosis.
Haematologica. 2024 Jul 1;109(7):2092-2110
HEC-59 cells
2.5, 5, 10, 20 μM
72 hours
To evaluate the effect of KJ-Pyr-9 on endometrial cancer cell viability, results showed that KJ-Pyr-9 inhibited cell viability in a dose-dependent manner.
Cells. 2021 Oct 27;10(11):2916
AN3CA cells
2.5, 5, 10, 20 μM
72 hours
To evaluate the effect of KJ-Pyr-9 on endometrial cancer cell viability, results showed that KJ-Pyr-9 inhibited cell viability in a dose-dependent manner.
Inhibition of MYC signaling significantly reduced the survival of ECSCs
Int J Mol Sci. 2022 Feb 22;23(5):2426
glioblastoma stem cells (GSCs)
40 µM
96 hours
Inhibition of MYC/MAX protein-protein interaction, significantly reducing GSC viability to 11.83%
Int J Mol Sci. 2022 Oct 26;23(21):12919
malignant mesothelioma cells
12.5 µM
30 hours
KJ-Pyr-9 alone or in combination with FRAX597 significantly enhanced apoptosis under serum starvation conditions
Am J Cancer Res. 2017 Aug 1;7(8):1724-1737
KJ Pyr 9 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Zebrafish
Tg(hsp70:E2A-PBX1-EGFP) transgenic zebrafish
Intraperitoneal injection
90 mg/kg
For 5 consecutive days
To evaluate the effect of KJ-Pyr-9 on hE2A-PBX1-induced AML-like disease in zebrafish, results showed that KJ-Pyr-9 significantly alleviated myeloid cell expansion.
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